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Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Development of novel benzotriazines for drug discovery
Moorthy Ss Palanki1, Jianguo Cao, Chun P Chow
1TargeGen, Inc., 9380 Judicial Drive, CA 92121, San Diego, USA +1 858 678 0760 ; +1 858 678 0762 ; Noronha@targegen.com.
Background:
The synthesis of novel benzotriazine heterocycles was developed independently around the same time by Bischler, Bamberger and Arndt. Over the years, different groups have reported the synthesis of benzotriazine based compounds.
Objective:
This literature review gives an update on recent benzotriazine compounds and their applications.
Conclusion:
The benzotriazine core has been used in various drug discovery projects including anticancer, anti-inflammatory and antimalarial programs. Recently, the benzotriazine core was used to develop selective kinase inhibitors targeting SRC, VEGFr2, BCR-ABL and BCR-ABL-T315I. Two benzotriazine based compounds, tirapazamine for the treatment of cancer and TG100801 for the treatment of age-related macular degeneration, have entered clinical trials.
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